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ID: ALA1146826

Journal: Bioorg Med Chem Lett

Title: A novel Pd-catalyzed cyclization reaction of ureas for the synthesis of dihydroquinazolinone p38 kinase inhibitors.

Authors: Schlapbach A, Heng R, Di Padova F.

Abstract: A series of potent p38 inhibitors based on the dihydroquinazoline scaffold was synthesized using a novel Pd-catalyzed cyclization reaction of aryl-benzyl ureas. Optimization of this compound class led to compound 20, which inhibits p38alpha in vitro with IC(50)=14 nM and is active in the mouse TNFalpha-release model.

CiteXplore: 14698158

DOI: 10.1016/j.bmcl.2003.11.006